In Vitro Activity of Sitafloxacin and Additional Newer Generation Fluoroquinolones Against Ciprofloxacin-Resistant Neisseria gonorrhoeae Isolates
In Vitro Activity of Sitafloxacin and Additional Newer Generation Fluoroquinolones Against Ciprofloxacin-Resistant Neisseria gonorrhoeae Isolates
复制标题
DOI：
10.1089/mdr.2017.0054
复制
发表时间：
2018-01-01
影响因子：
2.6
通讯作者：
Matsumoto, Tetsuro
中科院分区：
文献类型：
--
作者：
Hamasuna, Ryoichi;Ohnishi, Makoto;Matsumoto, Tetsuro
淋病奈瑟菌耐药性的出现是全球主要的公共卫生问题，治疗淋病的新抗生素势在必行。在这项研究中，确定了西他沙星（一种在日本主要用于呼吸道或泌尿生殖道感染的氟喹诺酮类药物）和其他新一代氟喹诺酮类药物对环丙沙星耐药奈瑟菌的体外活性。淋病分离株。环丙沙星、左氧氟沙星、利福沙星、西他氟沙星、帕珠沙星和托舒沙星对47 N.通过琼脂稀释法测定2009年在日本培养的淋病分离株。对gyrA和parC的喹诺酮类耐药决定区（QRDR）进行测序。与所有其他测试的氟喹诺酮类药物相比，西他布汀的体外效力显著更高。西他夫对35株环丙沙星耐药菌株的MIC为0.03 ~ 0.5mg/L。淋病分离株（环丙沙星MIC为2 - 32 mg/L）。在GyrA和ParC QRDR中没有发现导致西他夫MIC高于0.5mg/L的突变。西塔氟啶对N.淋病分离株，包括DNA促旋酶和拓扑异构酶IV突变的菌株，导致对环丙沙星和所有其他新一代氟喹诺酮类药物的高水平耐药性。然而，它仍然在较低程度上受到GyrA和ParC QRDR突变的影响，导致西他夫的MIC高达0.5mg/L。这表明西他夫胺不应被考虑作为淋病的经验性一线单药治疗。然而，西他夫利在双重抗菌治疗和头孢曲松耐药或过敏的病例中可能是有价值的。
Emergence of antimicrobial resistance in Neisseria gonorrhoeae is a major public health concern globally, and new antimicrobials for treatment of gonorrhea are imperative. In this study, the in vitro activity of sitafloxacin, a fluoroquinolone mainly used for respiratory tract or urogenital infections in Japan, and additional newer generation fluoroquinolones were determined against ciprofloxacin-resistant N. gonorrhoeae isolates. Minimum inhibitory concentrations (MICs) of ciprofloxacin, levofloxacin, moxifloxacin, sitafloxacin, pazufloxacin, and tosufloxacin against 47 N. gonorrhoeae isolates cultured in 2009 in Japan were determined by agar dilution method. The quinolone resistance-determining region (QRDR) of gyrA and parC was sequenced. The in vitro potency of sitafloxacin was substantially higher compared with all other tested fluoroquinolones. The MICs of sitafloxacin ranged from 0.03 to 0.5mg/L for 35 ciprofloxacin-resistant N. gonorrhoeae isolates (ciprofloxacin MICs from 2 to 32mg/L). No identified mutations in GyrA and ParC QRDR resulted in higher sitafloxacin MIC than 0.5mg/L. Sitafloxacin had a high activity against N. gonorrhoeae isolates, including strains with mutations in DNA gyrase and topoisomerase IV, resulting in high-level resistance to ciprofloxacin and all other newer generation fluoroquinolones examined. However, it was still to a lower extent affected by GyrA and ParC QRDR mutations resulting in sitafloxacin MICs of up to 0.5mg/L. This indicates that sitafloxacin should not be considered for empirical first-line monotherapy of gonorrhea. However, sitafloxacin could be valuable in a dual antimicrobial therapy and for cases with ceftriaxone resistance or allergy.